948713-76-6Relevant articles and documents
Design, step-economical diversity-oriented synthesis of an N-heterocyclic library containing a pyrimidine moiety: Discovery of novel potential herbicidal agents
Ma, Dong,Yin, Yang,Chen, Ying-Lu,Yan, Yi-Tao,Wu, Jun
, p. 15380 - 15386 (2021/05/19)
The synthesis of highly diverse libraries has become of paramount importance for obtaining novel leads for drug and agrochemical discovery. Herein, the step-economical diversity-oriented synthesis of a library of various pyrimidine-N-heterocycle hybrids was developed, in which a 4,6-dimethoxypyrimidine core was incorporated into nine kinds of N-heterocycles. A total of 34 structurally diverse compounds were synthesized via a two-step process from very simple and commercially available starting materials. Further, in vivo biological screening of this library identified 11 active compounds that exhibited good post-emergence herbicidal activity against D. sanguinalis at 750 g ai per ha. More importantly, pyrimidine-tetrahydrocarbazole hybrid 5q showed good to excellent herbicidal activity against five test weeds at the same dosage. Pyrimidine-tetrahydrocarbazole hybrids represent a novel class of herbicidal agents that may become promising lead compounds in the herbicidal discovery process.
Copper-catalyzed regioselective intramolecular oxidative α-functionalization of tertiary amines: An efficient synthesis of dihydro-1,3-oxazines
Deb, Mohit L.,Dey, Suvendu S.,Bento, Isabel,Barros, M. Teresa,Maycock, Christopher D.
supporting information, p. 9791 - 9795 (2013/09/23)
Traffic control: The hydroxy functional group directs the α-functionalization of tertiary amines, synthesizing 1,3-oxazines by C-O bond formation. Reaction occurs with both benzylic and non-benzylic amines. In the case of naphthoxazine synthesis, 100 % diastereoselectivity was observed. A tentative two-pathway mechanism is proposed for the reaction. Copyright
Tunable hydride transfer in the redox amination of indoline with aldehyde: An attractive intramolecular hydrogen-bond effect
Mao, Hui,Xu, Runsheng,Wan, Jieping,Jiang, Zhengyang,Sun, Cuirong,Pan, Yuanjiang
supporting information; experimental part, p. 13352 - 13355 (2011/03/17)
Hydride hijacked by "hydrogen"! N-Alkylindoles and N-alkylindolines were obtained in the redox amination of indoline with aldehyde, which was tuned by a hydrogen-bond effect. Salicylaldehyde gave the indoline-type product via intermolecular hydride transfer, while other aromatic aldehydes gave the indole-type product via intramolecular hydride transfer. Copyright
